epithelial-mesenchymal transition (emt)

Sulindac (Sulindac sulfoxide) 是一种非甾体类抗炎剂，可抑制COX-2的活性，也可抑制 COX-2 的过表达。它是一种亚磺酰基茚衍生物前药，具有潜在的抗肿瘤活性。

AXL-IN-13 是一种有效且具有口服活性的 AXL 抑制剂 ，其IC50值为 1.6 nM，Kd 值为0.26 nM。AXL-IN-13 具有抗癌活性，可逆转 TGF-β1 诱导的上皮间质转化 (EMT)，并抑制癌细胞迁移和侵袭。

Methacycline hydrochloride (Rondomycin) 是四环素抗生素，可抑制细菌蛋白质的合成。它是上皮-间质转化 (EMT) 抑制剂。它在体外可阻断 EMT，体内抑制纤维发生，不会直接影响 TGF-β1 Smad 信号传导。它是抗菌剂，有潜力研究肺纤维化。

EMT inhibitor-2 inhibits CYP3A4 testosteron and CYP2C9 with IC50s of 49.72 and 5.54 μM, respectively. EMT inhibitor-2 inhibits epithelial-mesenchymal transition (EMT) induced by substances such as IL-1β and TGF-β released from the immunocytes.

KY-05009 是 ATP 竞争性的、有效的 TNIK 抑制剂，Ki 为 100 nM。KY-05009抑制人肺腺癌细胞中 TGF-β1 诱导的上皮-间质转化。KY-05009 还抑制TNIK 的蛋白表达和Wnt 靶基因的转录活性，并诱导癌细胞凋亡，显示抗癌活性。

BPU17通过与PHB1结合，影响PHB1-PHB2间的相互作用，从而轻微损害线粒体功能。此类功能障碍进而抑制了SRF CArG-box依赖的转录过程，在体内抑制视网膜色素上皮细胞 (RPEs) 的上皮-间质转化 (EMT)，显示出明显的抗纤维化活性。因此，BPU17成为研究针对抗新生血管性年龄相关性黄斑变性 (nAMD) 的潜在试剂。

Methacycline，作为一种四环素类抗生素，具有抑制细菌蛋白质合成的功能。此外，它也是一种有效的上皮-间质转化(EMT)抑制剂，能在体外阻断EMT进程，并在体内抑制纤维化发生，但对TGF-β1Smad信号传递无直接影响。因其抗菌性和抑制纤维化的特性，Methacycline 在肺纤维化研究中显示出应用潜力。

HJ445A是一种高效选择性的MYOF抑制剂，具有良好的水溶性，用于治疗胃癌。在MGC803和MKN45胃癌细胞中，HJ445A具有强大的抗增殖能力，其IC50值分别为0.16 μM和0.14 μM。此外，HJ445A与MYOF-C2D结构域结合，其KD值为0.17 μM，且能够通过逆转上皮-间充质转化(EMT)过程阻止胃癌细胞的迁移，并以浓度依赖的方式抑制MKN45细胞的集落形成。值得注意的是，与化合物6y相比，HJ445A的水溶性得到了显著提高，增强了约170倍。此外，HJ445A在体内也显示出了卓越的抗肿瘤效果。

EMT inhibitor-3 (compound 11i) 是一种能够抑制上皮-间质转化 (EMT) 的化合物，对神经母细胞瘤 SK-N-SH 细胞的抑制IC50值为2.5 μM。它可抑制SK-N-SH细胞的增殖、迁移和侵袭，通过增加Bax Bcl-2蛋白表达比例促进细胞色素 (Cytochrome C) 从线粒体释放，并激活caspase 9和caspase 3，从而诱导线粒体介导的内源性细胞凋亡 (Apoptosis)。EMT inhibitor-3 可用于癌症研究。

AXL Angiokinase-IN-1 (compound 11b) 是一种对 AXL 三重血管激酶 (angiokinase) 的有效抑制剂，其 IC50 为 3.75 nM (AXL表达)。该化合物能抑制 Bxpc-3 的上皮间质转化 (EMT)，阻止肺癌细胞转移，并对血管和成纤维细胞的功能具有抑制作用，同时诱导癌细胞和成纤维细胞凋亡 (apoptosis)。此外，AXL Angiokinase-IN-1 还具有较低的毒性和良好的代谢稳定性。

FGFRs-IN-1 (Compound A16) 是一种有效的口服FGFR抑制剂，可分别抑制FGFR1、FGFR2、FGFR3和FGFR4，其IC50值为2.3、7、11和163 nM。此外，FGFRs-IN-1 同时抑制VEGFR1 2 3、Abl和Flt3，IC50值分别为61、176、112、26和353 nM，然而对CYP酶的抑制作用较弱。该化合物可降低α-SMA和胶原蛋白I (collagen I) 的表达，并在TGF-β1刺激的A549细胞中抑制上皮-间质转化 (EMT)。在Bleomycin诱导的小鼠肺纤维化模型及CCl4诱导的小鼠肝纤维化模型中，FGFRs-IN-1 显示出抗炎活性。

HPH-15 是一种抗细胞迁移化合物，其作用机制包括与hnRNP U结合或抑制TGF-β，从而抑制细胞迁移。此外，HPH-15 能抑制上皮到间充质转化 (EMT)，为抗肿瘤转移和抗纤维化研究提供了潜力。

Phthalazinone pyrazole 是强效、选择性和口服生物可利用的 Aurora-A 激酶抑制剂，IC50值为 0.031 μM。它抑制人胚胎干细胞向肝细胞样细胞分化过程中的上皮间质转化。它还可阻止有丝分裂并随后通过增殖细胞的凋亡抑制肿瘤生长。

CAY10736 is an anticancer compound.1 It inhibits proliferation in a panel of melanoma and breast, pancreatic, and lung cancer cell lines (IC50s = 0.827-9.89 μM). CAY10736 inhibits migration and epithelial-to-mesenchymal transition (EMT) of A375 and B16/F10 melanoma cells in vitro in a concentration-dependent manner. It reduces the viability of spheroid A375 and B16/F10 cells (IC50s = 2.4 and 1.59 μM, respectively) and increases the production of reactive oxygen species (ROS) in these cells in a concentration-dependent manner. CAY10736 (5 mg/kg) reduces tumor growth in B16/F10 melanoma and Lewis lung carcinoma mouse models and an A375 mouse xenograft model.References1. Liu, X., Li, B., Zhang, Z., et al. Synthesis and discovery novel anti-cancer stem cells compounds derived from the natural triterpenoic acids. J. Med. Chem. 61(23), 10814-10833 (2018). CAY10736 is an anticancer compound.1 It inhibits proliferation in a panel of melanoma and breast, pancreatic, and lung cancer cell lines (IC50s = 0.827-9.89 μM). CAY10736 inhibits migration and epithelial-to-mesenchymal transition (EMT) of A375 and B16/F10 melanoma cells in vitro in a concentration-dependent manner. It reduces the viability of spheroid A375 and B16/F10 cells (IC50s = 2.4 and 1.59 μM, respectively) and increases the production of reactive oxygen species (ROS) in these cells in a concentration-dependent manner. CAY10736 (5 mg/kg) reduces tumor growth in B16/F10 melanoma and Lewis lung carcinoma mouse models and an A375 mouse xenograft model. References1. Liu, X., Li, B., Zhang, Z., et al. Synthesis and discovery novel anti-cancer stem cells compounds derived from the natural triterpenoic acids. J. Med. Chem. 61(23), 10814-10833 (2018).

CAY10735 is an anticancer compound.1 It inhibits proliferation in a panel of melanoma and breast, pancreatic, and lung cancer cell lines (IC50s = 0.674-11.56 μM). CAY10735 inhibits migration of and the epithelial-to-mesenchymal transition (EMT) in A375 and B16 F10 melanoma cells in vitro in a concentration-dependent manner. It reduces the viability of spheroid A375 and B16 F10 cells (IC50s = 3.04 and 1.24 μM, respectively) and increases production of reactive oxygen species (ROS) in these cells in a concentration-dependent manner. CAY10735 (5 mg kg) reduces tumor growth in B16 F10 melanoma and Lewis lung carcinoma mouse models and an A375 mouse xenograft model.References1. Liu, X., Li, B., Zhang, Z., et al. Synthesis and discovery novel anti-cancer stem cells compounds derived from the natural triterpenoic acids. J. Med. Chem. 61(23), 10814-10833 (2018). CAY10735 is an anticancer compound.1 It inhibits proliferation in a panel of melanoma and breast, pancreatic, and lung cancer cell lines (IC50s = 0.674-11.56 μM). CAY10735 inhibits migration of and the epithelial-to-mesenchymal transition (EMT) in A375 and B16 F10 melanoma cells in vitro in a concentration-dependent manner. It reduces the viability of spheroid A375 and B16 F10 cells (IC50s = 3.04 and 1.24 μM, respectively) and increases production of reactive oxygen species (ROS) in these cells in a concentration-dependent manner. CAY10735 (5 mg kg) reduces tumor growth in B16 F10 melanoma and Lewis lung carcinoma mouse models and an A375 mouse xenograft model. References1. Liu, X., Li, B., Zhang, Z., et al. Synthesis and discovery novel anti-cancer stem cells compounds derived from the natural triterpenoic acids. J. Med. Chem. 61(23), 10814-10833 (2018).

EW-7195 是一种具有选择性和高效性的 ALK5 (TGFβR1) 抑制剂，IC50 值为 4.83 nM。EW-7195 对 ALK5 的亲和力是 p38α 的 300 多倍。EW-7195 对 TGF-β1 诱导的 Smad 信号转导、上皮间质转化 (EMT) 和乳腺癌向肺转移有抑制作用。

ML327 是 MYC 的阻断剂，还可抑制 E-钙粘蛋白转录和逆转上皮间质转化。

Sulindac (sodium) (MK-231) 是一种非甾体抗炎剂，具有口服活性。Sulindac (sodium) 用于减轻疼痛，肿胀和关节僵硬的关节炎。Sulindac 还用于脊柱关节炎、痛风性关节炎的研究。Sulindac (sodium) 作为一种免疫调节剂，可通过阻断 NF-κB 信号通路下调 PD-L1，调节 pMMR CRC 对抗 PD-L1 免疫治疗的应答，抑制结直肠癌 CRC 的发生发展。 Sulindac 还可通过下调 SIRT1 抑制 TGF-β1-诱导的 EMT，抑制肺癌细胞的迁移和侵袭。

Antitumor agent-77 对癌细胞的生长和迁移具有抑制作用，具有抗癌作用。Antitumor agent-77 能够抑制 GPx-4 和提高 COX2 引发铁下垂。Antitumor agent-77 可以激活肿瘤细胞固有凋亡通路 (Bax-Bcl-2-caspase-3)，阻碍肿瘤细胞上皮间质转化 (EMT) 过程。

CT1-3 是一种有效的抗癌剂。CT1-3 能够调控 JNK Bcl-2 Bax XIAP 通路，进而诱导线粒体介导的细胞凋亡 (apoptosis)。CT1-3 可以调控 E-cadherin Snail 轴抑制人癌细胞 (HCCs) 的上皮间充质转化 (EMT) 电位，并抑制肿瘤发生。CT1-3 在小鼠模型中具有抗肿瘤作用，且没有表现出明显的肝、肾毒性。

Antitumor agent-78 能够抑制 GPx-4 和升高 COX2 ，进而导致铁下垂 (ferroptosis)。Antitumor agent-78 可以激活肿瘤细胞固有凋亡通路 (Bax-Bcl-2-caspase-3)，抑制肿瘤细胞上皮间质转化 (EMT) 过程。Antitumor agent-78 表现出抗肿瘤效果，并能够抑制癌细胞的生长和迁移。

β-Carboline-1-carboxylic acid is an alkaloid that has been found in P. quassioides and has diverse biological activities. It reduces LPS-induced increases in MCP-1, TNF-α, IL-6, and IL-1β levels in RAW 264.7 cells when used at a concentration of 15 µg ml and inhibits the epithelial-to-mesenchymal transition (EMT) induced by TGF-β1 in A549 cells. β-Carboline-1-carboxylic acid induces cytotoxicity in CT26.WT, K562, and SGC-7901 cells (IC50s = 14.96, 22.11, and 19.7 µg ml, respectively) but not HepG2 or A549 cells (IC50s = 36.41 and 41.51 µg ml, respectively). It also inhibits cAMP phosphodiesterase with an IC50 value of 96 µM.

PI3K AKT-IN-2 是一种 PI3K 和 AKT 抑制剂。PI3K AKT-IN-2 阻断上皮-间质转化 (EMT)，诱导细胞凋亡 (apoptosis)。PI3K AKT-IN-2 抑制微管蛋白 (tubulin) 的聚合。

STAT3-IN-15是一款有效、具口服活性的STAT3抑制剂，用于对抗特发性肺纤维化（IPF）。该化合物阻止STAT3磷酸化，同时抑制TGF-β1引起的上皮细胞迁移及变形，并防止上皮间质转化（EMT）。